1047644-62-1Relevant articles and documents
Preparation method of Afuresertib
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Paragraph 0036-0039, (2020/09/08)
The invention discloses a preparation method of Afuresertib. The Afuresertib is prepared through an amidation reaction and an ammoniation reduction reaction between (2S)-2-amino-3-(3-fluorophenyl) methyl propionate and 5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxylic acid. The preparation method has the advantages of easily available raw materials, simple process, optimized environment and improved quality, and is suitable for industrial amplification requirements.
AFURESERTIB: Protein kinase B (PKB) inhibitor Oncolytic
Conkel,Benson
, p. 541 - 546 (2014/12/11)
The phosphatidylinositol 3-kinase (PI3K)/Akt/mammalian target of rapamycin (mTOR) signaling pathway plays key roles in cellular proliferation and survival. Mutations and alterations in this signal transduction pathway have been described in a variety of solid and hematopoietic malignancies, which may contribute to perpetuation of the disease in a number of ways. Increasing interest in targeting particular facets of this signaling cascade has led to the development of a number of novel anticancer agents, including afuresertib (GSK-2110183), an orally bioavailable pan-inhibitor of the RAC-alpha serine/threonine protein kinase, also referred to as protein kinase B or proto-oncogene c-Akt. The present review summarizes the preclinical and pharmacological aspects of afuresertib and early clinical experience.